The present invention, relates to the field of pharmacology and more particularly, but not exclusively, to novel oral dosage forms of oxidized phospholipids.
Oxidized phospholipids have been previously described as useful in the treatment of medical conditions such as, for example, cardiovascular diseases, cerebrovascular diseases and inflammatory diseases and disorders.
International Patent Application No. PCT/IL2004/000453 (Publication No. WO 04/106486), by the present assignee, describes oxidized lipids for prevention and treatment of inflammation associated with endogenous oxidized lipids. An exemplary such compound is described and known as CI-201 (1-hexadecyl-2-(4′-carboxybutyl)-glycero-3-phosphocholine), also referred to in the art as VB-201. VB-201 was found to be an orally active drug, useful in the treatment of inflammatory disorders such as atherosclerosis, psoriasis, multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease.
International Patent Application No. PCT/IL01/01080 (Publication No. WO 02/41827), by the present assignee, describes oxidized lipids for prevention and treatment of atherosclerosis and related diseases.
Additional background art includes International Patent Application Nos. PCT/IL05/000735 (Publication No. WO 06/006161), PCT/IL02/00005 (Publication No. WO 02/053092) and PCT/IL08/000,013 (Publication No. WO 08/084,472), all being also by the present assignee.
All of the above cited publications are incorporated by reference as if fully set forth herein.
Recently, and in view of the promising therapeutic effect of VB-201, clinical studies were conducted in order to evaluate the toxicity, efficacy and pharmacokinetic parameters of orally administered VB-201. The obtained results showed that daily dosages of 80 mg VB-201 per day or less are safe, well-tolerated, and effective at inhibiting inflammatory processes, that a substantial percentage of VB-201 is absorbed into the bloodstream, and that plasma concentrations of VB-201 are relatively stable when VB-201 is administered once per day, and are described in International Patent Application PCT/IL2011/000008, filed Jan. 5, 2011, which is incorporated by reference as if fully set forth herein.
In view of the potential therapeutic effects of oxidized phospholipids (e.g., VB-201), a need arises for industrially and pharmaceutically applicable formulations containing oxidized phospholipids, such as VB-201, as the active ingredient.